It is known that antifungal formulations for external use, more particularly, pharmaceutical compositions containing tolnaftate resistant to fungi and/or bacteria or imidazole derivatives such as clotrimazole, ketoconazole and the like having activity for candida species are generally available for the remedy of diseases related to the fungi including fungal infections.
Such known compositions have an excellent level of activity relative to a variety of microorganisms but, when substantially administrated through the skin of a patient, exhibit poor absorption and/or penetration into the horny layer of the skin, thereby resulting in unsatisfactory treatment. Moreover, when the conventional composition is applied to the skin, it is generally sticky causing an unpleasant feeling or discomfort. Therefore, it is required to improve the feeling or discomfort when appling the composition onto the skin.
Fluconazole, an antifungal active component, which has been developed for oral administration, is not practically used as a remedial formulation for external application.
Hereinbefore, an “oral” formulation means an agent which treats fungal disease by distributing the formulation into the internal parts of the entire body. Thus, for example, when a fluconazole based oral formulation is administered to treat a fungal disease excess dose of the formulation is required to obtain the desired curing value. However, long-term administration of triazole-based drugs may be a burden for the liver and cause undesired distribution for the drug through thereof over the entire body.
Accordingly, there is a pressing need to develop a novel remedial formulation for external use containing said fluconazole as a major active component in order to cure only the fungal infection of skin in a short period of time.